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NUAK family, SNF1-like kinase, 2

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Target id: 2130

Nomenclature: NUAK family, SNF1-like kinase, 2

Abbreviated Name: NuaK2

Family: NuaK subfamily

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 628 1q32.1 NUAK2 NUAK family kinase 2
Mouse - 639 1 E4 Nuak2 NUAK family, SNF1-like kinase, 2
Rat - 630 13q13 Nuak2 NUAK family kinase 2
Previous and Unofficial Names Click here for help
Omphalocele kinase 2 | OMPHK2 | SNARK | SNF1/AMP activated protein kinase | SNF1/AMP kinase-related kinase | UV126 | NUAK family
Database Links Click here for help
Alphafold Q9H093 (Hs), Q8BZN4 (Mm), Q66HE5 (Rn)
BRENDA 2.7.11.1
ChEMBL Target CHEMBL5698 (Hs)
Ensembl Gene ENSG00000163545 (Hs), ENSMUSG00000009772 (Mm), ENSRNOG00000000034 (Rn)
Entrez Gene 81788 (Hs), 74137 (Mm), 289419 (Rn)
Human Protein Atlas ENSG00000163545 (Hs)
KEGG Enzyme 2.7.11.1
KEGG Gene hsa:81788 (Hs), mmu:74137 (Mm), rno:289419 (Rn)
OMIM 608131 (Hs)
Pharos Q9H093 (Hs)
RefSeq Nucleotide NM_030952 (Hs), NM_001195025 (Mm), NM_001007617 (Rn)
RefSeq Protein NP_112214 (Hs), NP_001181954 (Mm), NP_001007618 (Rn)
UniProtKB Q9H093 (Hs), Q8BZN4 (Mm), Q66HE5 (Rn)
Wikipedia NUAK2 (Hs)
Enzyme Reaction Click here for help
EC Number: 2.7.11.1

Download all structure-activity data for this target as a CSV file go icon to follow link

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
WZ4003 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 7.0 pIC50 2
⤷ pIC50 7.0 (IC50 1x10-7 M) [2]
HTH-02-006 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 6.9 pIC50 5
⤷ pIC50 6.9 (IC50 1.26x10-7 M) [5]
Description: Determined in a radioactive (33P-ATP) filter-binding assay.
DiscoveRx KINOMEscan® screen Click here for help
A screen of 72 inhibitors against 456 human kinases. Quantitative data were derived using DiscoveRx KINOMEscan® platform.
http://www.discoverx.com/services/drug-discovery-development-services/kinase-profiling/kinomescan
Reference: 3-4
Key to terms and symbols Click column headers to sort
Target used in screen: SNARK
Ligand Sp. Type Action Value Parameter
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 10.1 pKd
lestaurtinib Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 9.0 pKd
NVP-TAE684 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 8.9 pKd
GSK-461364A Small molecule or natural product Hs Inhibitor Inhibition 7.6 pKd
fedratinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 7.3 pKd
KW-2449 Small molecule or natural product Hs Inhibitor Inhibition 7.3 pKd
midostaurin Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 7.2 pKd
tamatinib Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 7.2 pKd
GSK690693 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.1 pKd
crizotinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 6.9 pKd
Displaying the top 10 most potent ligands  View all ligands in screen »
EMD Millipore KinaseProfilerTM screen/Reaction Biology Kinase HotspotSM screen Click here for help
A screen profiling 158 kinase inhibitors (Calbiochem Protein Kinase Inhibitor Library I and II, catalogue numbers 539744 and 539745) for their inhibitory activity at 1µM and 10µM against 234 human recombinant kinases using the EMD Millipore KinaseProfilerTM service.

A screen profiling the inhibitory activity of 178 commercially available kinase inhibitors at 0.5µM against a panel of 300 recombinant protein kinases using the Reaction Biology Corporation Kinase HotspotSM platform.

http://www.millipore.com/techpublications/tech1/pf3036
http://www.reactionbiology.com/webapps/main/pages/kinase.aspx

Reference: ...1
Key to terms and symbols Click column headers to sort
Target used in screen: nd/SNARK(NUAK2)
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
Cdk1/2 inhibitor III Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 9.7
K-252a Small molecule or natural product Hs Inhibitor Inhibition 14.5
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 20.4
Cdk2 inhibitor IV Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 23.1
midostaurin Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 26.2
JNJ-7706621 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 34.0
Gö 6976 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 40.5
PKR inhibitor Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 41.2
JAK3 inhibitor VI Small molecule or natural product Hs Inhibitor Inhibition 43.7
SB 218078 Small molecule or natural product Hs Inhibitor Inhibition 52.0
Displaying the top 10 most potent ligands  View all ligands in screen »

References

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1. Anastassiadis T, Deacon SW, Devarajan K, Ma H, Peterson JR. (2011) Comprehensive assay of kinase catalytic activity reveals features of kinase inhibitor selectivity. Nat Biotechnol, 29 (11): 1039-45. [PMID:22037377]

2. Banerjee S, Buhrlage SJ, Huang HT, Deng X, Zhou W, Wang J, Traynor R, Prescott AR, Alessi DR, Gray NS. (2014) Characterization of WZ4003 and HTH-01-015 as selective inhibitors of the LKB1-tumour-suppressor-activated NUAK kinases. Biochem J, 457 (1): 215-25. [PMID:24171924]

3. Davis MI, Hunt JP, Herrgard S, Ciceri P, Wodicka LM, Pallares G, Hocker M, Treiber DK, Zarrinkar PP. (2011) Comprehensive analysis of kinase inhibitor selectivity. Nat Biotechnol, 29 (11): 1046-51. [PMID:22037378]

4. Wodicka LM, Ciceri P, Davis MI, Hunt JP, Floyd M, Salerno S, Hua XH, Ford JM, Armstrong RC, Zarrinkar PP et al.. (2010) Activation state-dependent binding of small molecule kinase inhibitors: structural insights from biochemistry. Chem Biol, 17 (11): 1241-9. [PMID:21095574]

5. Yuan WC, Pepe-Mooney B, Galli GG, Dill MT, Huang HT, Hao M, Wang Y, Liang H, Calogero RA, Camargo FD. (2018) NUAK2 is a critical YAP target in liver cancer. Nat Commun, 9 (1): 4834. [PMID:30446657]

How to cite this page

NuaK subfamily: NUAK family, SNF1-like kinase, 2. Last modified on 25/06/2020. Accessed on 18/04/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetomalariapharmacology.org/GRAC/ObjectDisplayForward?objectId=2130.